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Reversal Agents (reversal + agent)

Distribution by Scientific Domains

Medical Sciences	40%
Chemistry	40%

Selected Abstracts

ChemInform Abstract: Discovery of Highly Potent Multidrug Resistance (MDR) Reversal Agents: Aminosulfonylaryl Isoxazole Derivatives.

CHEMINFORM, Issue 36 2009
Young Taek Han
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]

Electrokinetic supercharging-electrospray ionisation-mass spectrometry for separation and on-line preconcentration of hypolipidaemic drugs in water samples

ELECTROPHORESIS, Issue 7 2010
Mohamed Dawod
Abstract Electrokinetic supercharging, a powerful on-line preconcentration technique in CE, was for the first time hyphenated with ESI-MS for the on-line concentration and separation of five hypolipidaemic drugs. The electrophoretic separation was performed in a co-EOF mode using the EOF reversal agent, hexadimethrine bromide, in ammonium bicarbonate electrolyte, pH 9.00. The ionic strength and the amount of methanol in the buffer were optimised in a multivariate manner using artificial neural networks, with the optimal conditions being 60,mM ammonium bicarbonate containing 60% methanol, providing baseline resolution of the five hypolipidaemics within 20,min. Using electrokinetic supercharging, the sensitivity of the method was improved 1000-fold over a conventional injection under field-amplified sample stacking conditions with LODs of 180,ng/L. This is the first report of the separation of hypolipidaemics by CE. The developed method was validated and then applied to the determination of the target drugs in water samples from Hobart city. [source]

Acceleromyography and mechanomyography for establishing potency of neuromuscular blocking agents: a randomized-controlled trial

ACTA ANAESTHESIOLOGICA SCANDINAVICA, Issue 4 2009
C. CLAUDIUS
Background: Acceleromyography (AMG) is increasingly being used in neuromuscular research, including in studies establishing the potency of neuromuscular blocking and reversal agents. However, AMG is insufficiently validated for use interchangeably with the gold standard, mechanomyography (MMG) for this purpose. The aim of this study was to compare AMG and MMG for establishing dose,response relationship and potency, using rocuronium as an example. Methods: We included 40 adult patients in this randomized-controlled single-dose response study. Anaesthesia was induced and maintained with propofol and opioid. Neuromuscular blockade was induced with rocuronium 100, 150, 200 or 250 ,g/kg. Neuromuscular monitoring was performed with AMG (TOF-Watch® SX) with pre-load (Hand Adapter) at one arm and MMG (modified TOF-Watch® SX) on the other, using 0.1 Hz single twitch stimulation. Dose,response relationships were determined for both recording methods using log (dose) against probit (maximum block). The obtained slopes of the regression lines, ED50, ED95 and the maximum block were compared. Results: The ED50 and ED95 [95% confidence interval (CI)] for AMG were 185 ,g/kg (167,205 ,g/kg) and 368 ,g/kg (288,470 ,g/kg), compared with 174 ,g/kg (159,191 ,g/kg) and 338 ,g/kg (273,418 ,g/kg) for MMG. There were no statistically significant biases in maximum block, ED50, ED95 or slopes obtained with the two methods. Conclusion: Our results indicate that any possible difference between AMG and MMG is so small that it justifies AMG to be used for establishing the potency of neuromuscular blocking agents. However, the wide CIs show that we cannot rule out a 13% higher ED50 and a 26% higher ED95 for AMG. [source]

Multidrug resistance in haematological malignancies

JOURNAL OF INTERNAL MEDICINE, Issue 5 2000
P. Sonneveld
Abstract. Sonneveld P (University Hospital Rotterdam , Dijkzigt, The Netherlands). Multidrug resistance in haematological malignancies (Internal Medicine in the 21st Century). J Intern Med 2000; 247: 521,534. The development of refractory disease in acute myeloid or lymphoblastic leukaemias (AML, ALL) and multiple myeloma (MM) is frequently associated with the expression of one or several multidrug resistance (MDR) genes. MDR1, MRP1 and LRP have been identified as important adverse prognostic factors in AML, T-ALL and MM. Recently, it has become possible to reverse clinical multidrug resistance by blocking P-glycoprotein-mediated drug efflux. The potential relevance of these reversal agents of MDR and potential new approaches to treat refractory disease are discussed. [source]

Anticancer multidrug resistance mediated by MRP1: Recent advances in the discovery of reversal agents

MEDICINAL RESEARCH REVIEWS, Issue 4 2005
Ahcène Boumendjel
Abstract Multidrug resistance protein 1 (MRP1) belongs to the ATP-binding cassette (ABC) transporter family. It is able to transport a broad range of anticancer drugs through cellular membranes, thus limiting their antiproliferative action. Since its discovery in 1992, MRP1 has been the most studied among MRP proteins, which now count nine members. Besides the biological work, which targets structure elucidation, binding sites location, and mode of action, most efforts have been focused on finding molecules which act as MRP1 inhibitors. In this review, we attempt to summarize and highlight studies dealing with modulators of MRP1-mediated multidrug resistance (MDR), which have been accomplished in the last 5 years. The reported MRP1 inhibitors are discussed according to their chemical class. Finally, we try to bring information on structure,activity relationship (SAR) aspects and how modulators might interact with MRP1. This study may facilitate the rational design of future modulators of MDR. © 2005 Wiley Periodicals, Inc. [source]